lmmol · Proteins

Gamma-aminobutyric acid type B receptor subunit 1

UniProt Q9UBS5 Organism Homo sapiens Gene GABBR1, GPRC3A

Also known as: GABBR1, GPRC3A

Function

Component of a heterodimeric G protein-coupled receptor for GABA, formed by GABBR1 and GABBR2. Within the heterodimeric GABA receptor, only GABBR1 seems to bind agonists, while GABBR2 mediates coupling to G proteins. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Signaling inhibits adenylate cyclase, stimulates phospholipase A2, activates potassium channels, inactivates voltage-dependent calcium-channels and modulates inositol phospholipid hydrolysis. Calcium is required for high affinity binding to GABA (By similarity). Plays a critical role in the fine-tuning of inhibitory synaptic transmission. Pre-synaptic GABA receptor inhibits neurotransmitter release by down-regulating high-voltage activated calcium channels, whereas postsynaptic GABA receptor decreases neuronal excitability by activating a prominent inwardly rectifying potassium (Kir) conductance that underlies the late inhibitory postsynaptic potentials. Not only implicated in synaptic inhibition but also in hippocampal long-term potentiation, slow wave sleep, muscle relaxation and antinociception (Probable). Activated by (-)-baclofen, cgp27492 and blocked by phaclofen.

Classification

Family (Pfam)
PF00003 7tm_3, PF01094 ANF_receptor, PF00084 Sushi
InterPro
ANF_lig-bd_rcpt, GPCR3_GABA-B, GPCR_3_C, GPCR_3_GABA_rcpt_B1, Peripla_BP_I, Sushi/SCR/CCP_sf, Sushi_SCR_CCP_dom
Functional cluster
Mixed Regulatory & Membrane Proteins

Experimental structures · PDB · 24

A predicted model is available from AlphaFold.

Gene Ontology · 35

Disease associations

Drugs targeting this protein · 9

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

Literature · 20 cited papers

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